Enantioselective synthesis of (R)-(-)-baclofen via Ru(II)-BINAP catalyzed asymmetric hydrogenation

A short and efficient enantioselective synthesis of (R)-(-)-baclofen, a selective GABA(B) agonist has been described with an overall yield of 26% and 90% ee. Ru(II)-(S)-BINAP catalyzed asymmetric hydrogenations of C=C and C=O groups constitute the key steps in introducing stereogenic centers into the molecule. (C) 2003 Elsevier Science Ltd. All rights reserved.